目的：比较RR-福莫特罗和rac-福莫特罗对人支气管舒张作用。方法：将内径2～4mm、长15mm的人支气管螺旋条置入持续供氧的浴槽内，静息张力为1g，以蓄积给药法测定RR-福莫特罗（10 pmol•L-1～3.2 Lmol•L-1）和rac-福莫特罗（10 pmol•L-1～3.2 Lmol•L-1）在静息情况下，及氨甲酰胆碱（10 Lmo l•L-1）或组胺（100 Lmol•L-1）引起收缩情况下的张力改变。结果：RR-福莫特罗在静息状况下支气管舒张作用强于rac-福莫特罗（P<0.05）。RR-福莫特罗和rac-福莫特罗对抗由氨甲酰胆碱和组胺引起的收缩，且RR-福莫特罗的对抗作用强于rac-福莫特罗（P<0.05）。结论：RR-福莫特罗对人支气管的舒张作用强于rac-福莫特罗。

human PDE4A was improved by ammonium sulfate fractionation, DEAE Sephadex A-50 chromatography, and Sephadex G-100 chromatography. The activity of PDE4A was measured by high performance liquid chromatography (HPLC). RESULTS: Induced PDE4A activity expressed in crude yeast cell GL62 supernatant and pellet was (340±21) nmol•g-1•min-1 and (250±25) nmol•g-1•min-1 respectively. The specific activity of recombinant PDE4A in supernatant was improved 6.4 fold. Ciclamilast, piclamilast, and rolipram could inhibit PDE4A activity. The IC50 values (95% confidence limits) of ciclamilast, piclamilast, and rolipram were 1.27 (0.84-1.91), 66.4 (33.3-132.2), and 3.73 (2.51-5.53) μmol/L respectively. Zaprinast, aspirin, and indomethacin had no obvious inhibitory effect on PDE4A activity. CONCLUSION: The specific activity of PDE4A expressed in yeast cell GL62 can be improved by ammonium sulfate fractionation, DEAE Sephadex A-50 chromatography, and Sephadex G-100 chromatography. Ciclamilast, piclamilast, and rolipram can inhibit PDE4A activity while zaprinast, aspirin, and indomethacin have no obvious inhibitory effect on PDE4A activity. Human PDE4A expressed in GL62 might be useful in the research and screening of new selective PDE4 inhibitors.

支气管哮喘（以下简称哮喘） 是呼吸系统疾病中的一种常见病，现在认为哮喘是气道慢性炎症性疾病，以肺部可逆性气流阻塞、气道黏膜炎症和气道高反应性为特征。近年来，主要在磷酸二酯酶、磷脂酶D、中枢神经系统在哮喘发病过程中的神经免疫调节作用和新药开发等方面进行了研究，并建立了相应的实验研究方法，为今后进一步的研究工作打下坚实基础。

To study the inductive expression of human phosphodiesterase 4A (hPDE4A) in yeast cell GL62 and investigate the inhibitory effects of theophylline, rolipram, and acetamide-45 on PDE4A activity of the expressed product in yeast cell GL62. METHODS: Yeast cell GL62 were transfected with human PDE4A gene cloned in the expression plasmid p138NB. Expression was induced by adding CuSO4 to a final concentration of 150μmol/L, and the expressed product was extracted. The activity of PDE4A was detected by HPLC. RESULTS: Yeast cell GL62 expressed a certain protein at CuSO4 150μmol/L, the size of the expressed product was between 62 kDa and 83 kDa, the activity of PDE4A of the expressed product at 3 h was in maximum (188±23)μmol×g-1×min-1, and the Km was (17.7±2.6) mmol/L. Theophylline, rolipram, and acetamide-45 could inhibit the activity of PDE4A extracted from yeast cell GL62. The IC50 (95% confidence limits) of theophylline, rolipram, and acetamide-45 were 1642 (989-2727), 4.58 (3.45-6.08), and 275 (170-444) mmol/L respectively. CONCLUSION: PDE4A expressed in yeast cell GL62 is biologically active. Theophylline, rolipram, and acetamide-45 can inhibit the PDE4A activity. The expressed product in yeast cell GL62 may be used in the research work of PDE4 and its inhibitors.

探讨隐孔菌发酵物（Cryp top orus volvatus ferment substance, CVFS）对中性粒细胞释放白三烯的影响。方法：给大鼠腹腔注射糖原诱导中性粒细胞聚集，16h后收集腹腔灌洗液，分离中性粒细胞，以calcium ionopho re A 23187刺激离体中性粒细胞释放白三烯，再用HPLC法测定中性粒细胞中白三烯（LT）B4、L TC4和LTD4的含量。结果：CVFS 0.25、1、4mg•L-1呈浓度依赖抑制中性粒细胞释放LTB4、LTC4和LTD4，对LTB4抑制率分别为27.4%、54.2%和78.8%；对LTC4抑制率分别为65.1%、74.3 和79.0%；对LTD4抑制率分别为5516%、60.9%和72.8%。与生理盐水对照组比较有显著性差异（P<0.05）。结论：CVFS抑制中性粒细胞释放LTB4、LTC4和LTD4可能是其抗炎平喘作用机制之一。